ACTIONS OF POLYPHENOLIC COMPOUNDS ON
GLUTAMATE-BINDING SITES OF THE NMDA RECEPTOR
SYNAPTOSOME IN THE RAT BRAIN
Khoshimov N.N., Rakhimova G.L., Mukhtorov A.A., Rakhimov R.N.
Institute of Biophysics and Biochemistry
at the National University of Uzbekistan,
Namangan State University,
Institute of Bioorganic Chemistry named after acad. A. Sadykov
Academy of Sciences of Uzbekistan,
Tashkent, Uzbekistan
Academic supervisor: Nasirov K.E., D. sci. (Biology), Prof.
Calcium ions have unique properties and a universal ability to conduct
a variety of signals that have a primary effect on the cell. In each of the
body’s signal transduction systems, Ca
2+
ions are important as a secondary
mediator. Calcium is an effective regulator of metabolic processes in
all cells, where there are systems that respond to small changes in its
concentration. Calcium has long been known as an important link in
synaptic transmission. Depolarization of the presynaptic nerve ending
during the action potential opens voltage-gated calcium channels through
which calcium enters the cell and triggers the release of the mediator from
the vesicles.
The effect of polyphenolic compound 7 (PC-7) on the neurotransmitter
system of NMDA receptors in the membranes of rat brain synaptosomes
was studied.
The synaptosomes were purified from the rat brain by two-stage
centrifugation. Measure the amount of intracellular calcium [Ca
2+
]in was
calculated by the Grinkevich equation.
In the presence of chlortetracycline (CTC) in the incubation medium,
glutamate at a concentration of 50 μM increases the level of fluorescence,
which indicates an increase in the concentration of Ca
2+
in the cytosol
[Ca
2+
]in, caused by glutamate, due primarily to [Ca
2+
]in. Pre- the
fluorescence level, then the addition of glutamate (50 μM) reduced the
fluorescence and, accordingly, the level of [Ca
2+
]in in synaptosomes. The
activity of the modulating effect of PC-7 on glutamate with synaptosomes
692
ФАРМАКОЛОГИЯ, ФАРМАКОГНОЗИЯ, ФАРМАЦЕВТИКА, ТОКСИКОЛОГИЯ
in rat brains was assessed in two ways: based on the bound glutamate on
the concentration of PC-7 and study of the kinetics of glutamate binding
in the presence of PC-7. Studies have shown that PC-7 effectively inhibits
glutamate. The practical significance of the research results lies in the fact
that the methods used and the identified mechanisms will serve as the
basis for the determination of new neuroprotective compounds in order
to create drugs and can be used as activators and inhibitors of the calcium
channels of the nerve cell.
ФАРМАКОЛОГИЯ, ФАРМАКОГНОЗИЯ, ФАРМАЦЕВТИКА, ТОКСИКОЛОГИЯ
693
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